3-amino-N-(3-aminopropyl)propanamide | 97614-99-8

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 3-amino-N-(3-aminopropyl)propanamide
• CAS: 97614-99-8
• 化学式: C₆H₁₅N₃O
• 分子量: 145.205
• InChiKey: ZFPLMJPIOLTOLB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2
• 重原子数：
  10
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  81.1
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  9-氯吖啶 、 3-amino-N-(3-aminopropyl)propanamide 在 苯酚 作用下， 反应 2.0h， 生成 Propanamide, 3-(9-acridinylamino)-N-(3-(9-acridinylamino)propyl)-
  参考文献：
  名称：

  Potential antitumor agents. 44. Synthesis and antitumor activity of new classes of diacridines: importance of linker chain rigidity for DNA binding kinetics and biological activity

  摘要：

  Four classes of diacridines, joined at the 9-position by linker chains of varying length, rigidity, and polarity, were evaluated for DNA-binding properties and antitumor activity. Diacridines linked by flexible chains of varying polarity show relatively fast chromophore exchange kinetics among DNA binding sites but slower dissociation rates, suggesting the potential for considerable "creeping" of the drug along the helix, and are inactive in vivo. The exchange kinetics can be slowed dramatically by inclusion of positive charges in the side chain, but the resulting polycationic drugs are inactive in vivo, possibly due to poor distribution. Diacridines linked by a rigid, polar but neutral dicarbamoylpyrazole chain retain slow exchange kinetics, have a greatly reduced potential "creep rate", and possess good in vitro potency and significant in vivo antileukemic activity.

  DOI：

  10.1021/jm00149a005
• 作为产物：
  描述：

  benzyl N-[3-oxo-3-[3-(phenylmethoxycarbonylamino)propylamino]propyl]carbamate 在 palladium on activated charcoal 氢气 作用下， 以 甲醇 为溶剂， 反应 8.0h， 以100%的产率得到3-amino-N-(3-aminopropyl)propanamide
  参考文献：
  名称：

  Potential antitumor agents. 44. Synthesis and antitumor activity of new classes of diacridines: importance of linker chain rigidity for DNA binding kinetics and biological activity

  摘要：

  Four classes of diacridines, joined at the 9-position by linker chains of varying length, rigidity, and polarity, were evaluated for DNA-binding properties and antitumor activity. Diacridines linked by flexible chains of varying polarity show relatively fast chromophore exchange kinetics among DNA binding sites but slower dissociation rates, suggesting the potential for considerable "creeping" of the drug along the helix, and are inactive in vivo. The exchange kinetics can be slowed dramatically by inclusion of positive charges in the side chain, but the resulting polycationic drugs are inactive in vivo, possibly due to poor distribution. Diacridines linked by a rigid, polar but neutral dicarbamoylpyrazole chain retain slow exchange kinetics, have a greatly reduced potential "creep rate", and possess good in vitro potency and significant in vivo antileukemic activity.

  DOI：

  10.1021/jm00149a005

文献信息

• Intranasal cyclic peptide formulations
  申请人：——

  公开号：US20010038824A1

  公开（公告）日：2001-11-08

  The present invention relates to a nasally administrable composition of a physiologically active cyclic peptide and pharmaceutically acceptable salts thereof that is prepared by homogeneously dispersing a physiologically active cyclic peptide such as antifungal cyclic peptides (aerothricins, echinocandin analogs, pneumocandin analogs, and aureobacidines), antibacterial cyclic peptides (e.g. vancomycin, daptomycin), cyclosporin A, lanreotide, vapreotide, vasopressin antagonist (U.S. Pat. No. 5,095,003) and eptifibatide in unique carrier, i.e. a physiologically acceptable powdery or crystalline carrier containing a water insoluble polyvalent metal carrier, or organic carrier having a mean particle size of 20 to 500 &mgr;m, in the presence or absence of an absorption enhancer and by homogeneously adsorbing onto the carrier, and its use for therapeutic treatment of disease such as systemic fungal infections by intranasal administration. The composition can be nasally administered in powder form.

  本发明涉及一种鼻腔可给药的生理活性环肽及其药学上可接受的盐的组合物，该组合物通过将生理活性环肽（如抗真菌环肽（气菌素、伊曲康定类似物、肺孢子菌素类似物和金黄色细菌素）、抗菌环肽（如万古霉素、达托霉素）、环孢霉素A、兰雷罗肽、瓦普雷罗肽、抗利尿激素拮抗剂（美国专利号5,095,003）和依普利贝肽）均匀分散在独特的载体中制备而成，即含有水不溶性多价金属载体或平均粒径为20至500微米的有机载体的生理上可接受的粉状或结晶载体中，存在或不存在吸收增强剂，通过均匀吸附到载体上，并用于通过鼻内给药治疗疾病，如系统真菌感染。该组合物可以以粉剂形式鼻腔给药。
• DENNY, W. A.;ATWELL, G. J.;BAGULEY, B. C.;WAKALIN, L. P. G., J. MED. CHEM., 1985, 28, N 11, 1568-1574
  作者：DENNY, W. A.、ATWELL, G. J.、BAGULEY, B. C.、WAKALIN, L. P. G.

  DOI：——

  日期：——
• AEROTHRICIN ANALOGS, THEIR PREPARATION AND USE
  申请人：F. HOFFMANN-LA ROCHE AG

  公开号：EP1100816A1

  公开（公告）日：2001-05-23
• NASALLY ADMINISTRABLE ANTIFUNGAL CYCLIC PEPTIDE COMPOSITIONS
  申请人：Basilea Pharmaceutica AG

  公开号：EP1251827B1

  公开（公告）日：2004-05-26
• NASALLY ADMINISTRABLE CYCLIC PEPTIDE COMPOSITIONS
  申请人：Basilea Pharmaceutica AG

  公开号：EP1251827A2

  公开（公告）日：2002-10-30